申请人:RESEARCH TRIANGLE PHARMACEUTICALS LTD.
公开号:EP0268222A2
公开(公告)日:1988-05-25
This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula
wherein X may represent sulfur, oxygen or nitrogen; a and b may be 0 or 1, c may be 0, 1 or 2, except that when X is oxygen, a, b and c are 0, when X is nitrogen c is 0 and only one of a or b is 1, and when X is sulfur a and b are0; A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; Rʹ is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl; and R is hydrogen or a lower alkyl group having from 1 to 4 carbon atoms,
wherein Rʺ is H or halogen, and salts, e.g. acid or quaternary derivatives, thereof. These compositions are useful in topical or transdermal applications of the physiologically-active agent.
本发明涉及一种在透皮装置或制剂中通过人和动物的皮肤或粘膜施用全身活性剂(包括治疗剂)的方法,包括与所述全身活性剂一起局部施用有效量的膜渗透促进剂,其结构式为
其中 X 可以代表硫、氧或氮;a 和 b 可以是 0 或 1,c 可以是 0、1 或 2,但当 X 是氧时,a、b 和 c 是 0,当 X 是氮时,c 是 0,a 或 b 中只有一个是 1,当 X 是硫时,a 和 b 是 0;A 是具有 0 至 2 个双键的支链或直链二价脂族基;Rʹ 选自由 H、具有 1 至 4 个碳原子的低级烷基、苯基、低级烷基或卤素取代的苯基、乙酰氨基、卤素、哌啶基、低级烷基或卤素取代的哌啶基、碳烷氧基、羧酰胺和烷酰基组成的组;以及 R 是氢或具有 1 至 4 个碳原子的低级烷基、
其中 Rʺ 是氢或卤素,以及它们的盐,如酸或季衍生物。这些组合物可用于生理活性剂的局部或透皮应用。